General Information of Drug (ID: DMKUE8O)

Drug Name
RP5063 Drug Info
Indication
Disease Entry ICD 11 Status REF
Schizophrenia 6A20 Phase 2 [1]
Alzheimer disease 8A20 Phase 1 [2]
Attention deficit hyperactivity disorder 6A05.Z Phase 1 [2]
Bipolar disorder 6A60 Phase 1 [2]
Major depressive disorder 6A70.3 Phase 1 [2]
Parkinson disease 8A00.0 Phase 1 [2]
Cross-matching ID
TTD Drug ID
DMKUE8O

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Preclinical Drug(s)
Patented Agent(s)
Investigative Drug(s)
Drug(s) Targeting Dopamine D3 receptor (D3R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cariprazine DMJYDVK Bipolar disorder 6A60 Approved [4]
Pramipexole DMNMW9R Parkinson disease 8A00.0 Approved [5]
Ropinirole DMA6S1D Parkinson disease 8A00.0 Approved [5]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [6]
P2B-001 DM9PVHX Parkinson disease 8A00.0 Phase 3 [7]
ONC201 DMM5SCF Endometrial cancer 2C76 Phase 2 [8]
TAK-906 DMBQD9H Diabetic gastroparesis DA41.00 Phase 2 [9]
GSK598809 DMGU05N Drug abuse 6C4G.1Z Phase 2 [10]
GSK618334 DMJPXZ4 Drug abuse 6C4G.1Z Phase 1 [10]
Pfizer 10 DM6ER9L Female sexual arousal dysfunction HA01.1 Phase 1 [11]
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Drug(s) Targeting Dopamine D4 receptor (D4R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Clozapine DMFC71L Schizophrenia 6A20 Approved [5]
Phenyltoloxamine DMKAEQW Allergy 4A80-4A85 Approved [12]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [6]
L-745,870 DMTGR25 Psychotic disorder 6A20-6A25 Phase 2 [13]
NGD 94-1 DMM1Y8F Schizophrenia 6A20 Phase 1 [14]
ABT-724 DMDQVY4 Erectile dysfunction HA01.1 Discontinued in Phase 2 [15]
Lu-35138 DMQ7A35 Psychotic disorder 6A20-6A25 Discontinued in Phase 2 [16]
NGD-94-4 DMZ9WLO Schizophrenia 6A20 Discontinued in Phase 1 [17]
PD-165167 DMD0GB4 Schizophrenia 6A20 Preclinical [14]
SPI-376 DMC1WAJ Schizophrenia 6A20 Preclinical [14]
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Drug(s) Targeting 5-HT 2A receptor (HTR2A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [18]
ZOTEPINE DMF3VXA Anxiety disorder 6B00-6B0Z Approved [19]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [20]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [4]
Lurasidone hydrochloride DMCVPXO Schizophrenia 6A20 Approved [21]
Aniracetam DMOIFW0 Cerebrovascular ischaemia 8B1Z Approved [22]
lumateperone tosylate DMQ8HOJ Schizophrenia 6A20 Approved [23]
Sarpogrelate DMGLP6S Diabetic complication 5A2Y Approved [24]
Pimavanserin DMR7IVC Parkinson disease 8A00.0 Approved [25]
Zicronapine DMP8ESD Schizophrenia 6A20 Phase 3 [26]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Dasotraline DMLDQFV Attention deficit hyperactivity disorder 6A05.Z Approved [2]
OPC-64005 DMIK2AD Attention deficit hyperactivity disorder 6A05.Z Phase 2 [27]
Brilaroxazine DM90J3J Idiopathic pulmonary fibrosis CB03.4 Phase 1 [28]
Drug(s) Targeting Dopamine D2 receptor (D2R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [29]
Haloperidol DM96SE0 Delirium Approved [30]
Perphenazine DMA4MRX Schizophrenia 6A20 Approved [31]
Perazine DM2AOTZ Psychotic disorder 6A20-6A25 Approved [32]
Domperidone DMBDPY0 Gastrointestinal disease DE2Z Approved [33]
Levodopa DMN3E57 Parkinson disease 8A00.0 Approved [34]
Quetiapine DM1N62C Anorexia nervosa cachexia 6B80 Approved [35]
Pimozide DMW83TP Schizophrenia 6A20 Approved [36]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [37]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [20]
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Drug(s) Targeting Histamine H1 receptor (H1R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [38]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [39]
Azelastine DMXTMBJ Allergic conjunctivitis 9A60.02 Approved [40]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [41]
Cinnarizine DM7U5QJ Meniere disease AB31.0 Approved [42]
Diphenhydramine DMKQTBA Hyperemesis gravidarum Approved [40]
Doxepin DMPI98T Anxiety Approved [43]
Chlorpheniramine DM5URA2 Allergic rhinitis CA08.0 Approved [40]
Epinastine DMX0K3Q Allergic conjunctivitis 9A60.02 Approved [44]
Desloratadine DM56YN7 Allergic rhinitis CA08.0 Approved [45]
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Drug(s) Targeting 5-HT 1A receptor (HTR1A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Trazodone DMK1GBJ Depression 6A70-6A7Z Approved [5]
Buspirone DMBS632 Anxiety disorder 6B00-6B0Z Approved [46]
OPC-34712 DMHG57U Major depressive disorder 6A70.3 Approved [47]
Vilazodone DM4LECQ Major depressive disorder 6A70.3 Approved [48]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [4]
Gepirone DMGX5Q0 Major depressive disorder 6A70.3 Approved [49]
TERTATOLOL DM2L3D5 Hypertension BA00-BA04 Approved [50]
Urapidil DMD59GI Hypertension BA00-BA04 Approved [51]
Treximet DMU54QB Migraine 8A80 Approved [10]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [6]
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Drug(s) Targeting 5-HT 7 receptor (HTR7)
Drug Name Drug ID Indication ICD 11 Highest Status REF
JNJ-18038683 DMV1T59 Major depressive disorder 6A70.3 Phase 2 [52]
AVN-101 DMOGFNI Cognitive impairment 6D71 Phase 2 [53]
ATI-9242 DM6GKMU Schizophrenia 6A20 Phase 1 [54]
PMID30124346-Compound-34TABLE4 DM2G3VE Attention deficit hyperactivity disorder 6A05.Z Patented [55]
PMID30124346-Compound-13TABLE4 DMHTJVA Attention deficit hyperactivity disorder 6A05.Z Patented [55]
Carbamide derivative 2 DMW5GI3 N. A. N. A. Patented [56]
4-oxadiazole derivative 1 DMWFHKR N. A. N. A. Patented [56]
SB-269970 DM8WTGA Sleep-wake disorder 7A00-7B2Z Terminated [57]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one DMM9X0G Discovery agent N.A. Investigative [58]
(+/-)-nantenine DM0L3GE Discovery agent N.A. Investigative [59]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 1A receptor (HTR1A) TTSQIFT 5HT1A_HUMAN Antagonist [3]
5-HT 2A receptor (HTR2A) TTJQOD7 5HT2A_HUMAN Partial agonist [2]
5-HT 7 receptor (HTR7) TTO9X1H 5HT7R_HUMAN Partial agonist [2]
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Antagonist [3]
Dopamine D3 receptor (D3R) TT4C8EA DRD3_HUMAN Partial agonist [2]
Dopamine D4 receptor (D4R) TTE0A2F DRD4_HUMAN Partial agonist [2]
Histamine H1 receptor (H1R) TTTIBOJ HRH1_HUMAN Partial agonist [2]
Serotoninnorepinephrinedopamine reuptake (SNDR) TT8G3Z7 NOUNIPROTAC Partial agonist [2]

References

1 ClinicalTrials.gov (NCT01490086) RP5063 in Subjects With Schizophrenia or Schizoaffective Disorder. U.S. National Institutes of Health.
2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 Drug Development in Schizophrenia: Summary and Table. Pharmaceutical Medicine October 2014, Volume 28, Issue 5, pp 265-271
4 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
6 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
7 Pharmacology of pramipexole, a dopamine D3-preferring agonist useful in treating Parkinson's disease. Clin Neuropharmacol. 1998 May-Jun;21(3):141-51.
8 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
9 Safety, Pharmacokinetics, and Pharmacodynamics of Trazpiroben (TAK-906), a Novel Selective D 2 /D 3 Receptor Antagonist: A Phase 1 Randomized, Placebo-Controlled Single- and Multiple-Dose Escalation Study in Healthy Participants. Clin Pharmacol Drug Dev. 2021 Jan 18.
10 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
11 Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66.
12 Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 ... J Med Chem. 2004 Aug 12;47(17):4155-8.
13 Dopamine D4 receptor involvement in the discriminative stimulus effects in rats of LSD, but not the phenethylamine hallucinogen DOI. Psychopharmacology (Berl). 2009 Apr;203(2):265-77.
14 The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
15 Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats. Proc Natl Acad Sci U S A. 2004 April 27; 101(17): 6758-6763.
16 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014237)
17 I. NGD 94-1: identification of a novel, high-affinity antagonist at the human dopamine D4 receptor. J Pharmacol Exp Ther. 1997 Aug;282(2):1011-9.
18 Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23.
19 Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
20 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
21 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
22 Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism. Eur J Pharmacol. 2001 May 18;420(1):33-43.
23 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
24 Beneficial effects of sarpogrelate hydrochloride, a 5-HT2A receptor antagonist, supplemented with pioglitazone on diabetic model mice. Endocr Res. 2009;34(1-2):18-30.
25 Pimavanserin, a selective serotonin (5-HT)2A-inverse agonist, enhances the efficacy and safety of risperidone, 2mg/day, but does not enhance efficacy of haloperidol, 2mg/day: comparison with reference dose risperidone, 6mg/day.Schizophr Res.2012 Nov;141(2-3):144-52.
26 Clinical pipeline report, company report or official report of Lundbeck.
27 Clinical pipeline report, company report or official report of Otsuka Pharmaceutical.
28 Clinical pipeline report, company report or official report of Reviva Pharmaceuticals
29 The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74.
30 Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
31 CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
32 Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.
33 Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
34 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3639).
35 Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
36 [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
37 Modulatory role of dopamine D2 receptors and fundamental role of L-type Ca2+ channels in the induction of long-term potentiation in the basolateral... Eur J Pharmacol. 2009 Mar 15;606(1-3):90-3.
38 Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
39 Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
40 Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79.
41 Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
42 Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
43 Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
44 Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cell... Mediators Inflamm. 2009;2009:738038.
45 Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
46 Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
47 Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors.Pharmacol Biochem Behav.2014 Sep;124:245-9.
48 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
49 Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
50 Synthesis of new derivatives of 8-OH-DPAT: Influence of substitution on the aromatic ring on the pharmacological profile, Bioorg. Med. Chem. Lett. 3(10):2035-2038 (1993).
51 Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
52 Selective pharmacological blockade of the 5-HT7 receptor attenuates light and 8-OH-DPAT induced phase shifts of mouse circadian wheel running activity. Front Behav Neurosci. 2015 Jan 15;8:453.
53 AVN-101: A Multi-Target Drug Candidate for the Treatment of CNS Disorders. J Alzheimers Dis. 2016 May 25;53(2):583-620.
54 Pharmacological characteristics of ATI-9242, a Novel Atypical Antipsychotic. FASEB J, April, 2010, 24(Meeting Abstract Supplement),773.12.
55 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.
56 Acyltransferase inhibitors: a patent review (2010-present).Expert Opin Ther Pat. 2015 Feb;25(2):145-58.
57 [(3)H]-SB-269970--A selective antagonist radioligand for 5-HT(7) receptors. Br J Pharmacol. 2000 May;130(2):409-17.
58 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
59 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.